Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy

Christopher F. Thompson; Nazia Quraishi; Amjad Ali; James R. Tata; Milton L. Hammond; James M. Balkovec; Monica Einstein; Lan Ge; Georgianna Harris; Theresa M. Kelly; Paul Mazur; Shilpa Pandit; Joseph Santoro; Ayesha Sitlani; Chuanlin Wang; Joanne Williamson; Douglas K. Miller; Ting Ting D. Yamin; Chris M. Thompson; Edward A. O'Neill; Dennis Zaller; Michael J. Forrest; Ester Carballo-Jane; Silvi Luell

doi:10.1016/j.bmcl.2005.02.009

Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy

Christopher F. Thompson
, Nazia Quraishi
, Amjad Ali
, James R. Tata
, Milton L. Hammond
, James M. Balkovec
, Monica Einstein
, Lan Ge
, Georgianna Harris
, Theresa M. Kelly
, Paul Mazur
, Shilpa Pandit
, Joseph Santoro
, Ayesha Sitlani
, Chuanlin Wang
, Joanne Williamson
, Douglas K. Miller
, Ting Ting D. Yamin
, Chris M. Thompson
, Edward A. O'Neill

Dennis Zaller, Michael J. Forrest, Ester Carballo-Jane, Silvi Luell

Center for Discovery and Innovation

Merck

Research output: Contribution to journal › Article › peer-review

42 Scopus citations

Abstract

A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

Original language	English
Pages (from-to)	2163-2167
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2005.02.009
State	Published - 15 Apr 2005

Keywords

Dissociation
Glucocorticoid
Inflammation
Transactivation
Transrepression

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10.1016/j.bmcl.2005.02.009

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Thompson, C. F., Quraishi, N., Ali, A., Tata, J. R., Hammond, M. L., Balkovec, J. M., Einstein, M., Ge, L., Harris, G., Kelly, T. M., Mazur, P., Pandit, S., Santoro, J., Sitlani, A., Wang, C., Williamson, J., Miller, D. K., Yamin, T. T. D., Thompson, C. M., ... Luell, S. (2005). Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy. Bioorganic and Medicinal Chemistry Letters, 15(8), 2163-2167. https://doi.org/10.1016/j.bmcl.2005.02.009

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title = "Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy",

abstract = "A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.",

keywords = "Dissociation, Glucocorticoid, Inflammation, Transactivation, Transrepression",

author = "Thompson, \{Christopher F.\} and Nazia Quraishi and Amjad Ali and Tata, \{James R.\} and Hammond, \{Milton L.\} and Balkovec, \{James M.\} and Monica Einstein and Lan Ge and Georgianna Harris and Kelly, \{Theresa M.\} and Paul Mazur and Shilpa Pandit and Joseph Santoro and Ayesha Sitlani and Chuanlin Wang and Joanne Williamson and Miller, \{Douglas K.\} and Yamin, \{Ting Ting D.\} and Thompson, \{Chris M.\} and O'Neill, \{Edward A.\} and Dennis Zaller and Forrest, \{Michael J.\} and Ester Carballo-Jane and Silvi Luell",

year = "2005",

month = apr,

day = "15",

doi = "10.1016/j.bmcl.2005.02.009",

language = "English",

volume = "15",

pages = "2163--2167",

journal = "Bioorganic and Medicinal Chemistry Letters",

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Thompson, CF, Quraishi, N, Ali, A, Tata, JR, Hammond, ML, Balkovec, JM, Einstein, M, Ge, L, Harris, G, Kelly, TM, Mazur, P, Pandit, S, Santoro, J, Sitlani, A, Wang, C, Williamson, J, Miller, DK, Yamin, TTD, Thompson, CM, O'Neill, EA, Zaller, D, Forrest, MJ, Carballo-Jane, E & Luell, S 2005, 'Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy', Bioorganic and Medicinal Chemistry Letters, vol. 15, no. 8, pp. 2163-2167. https://doi.org/10.1016/j.bmcl.2005.02.009

TY - JOUR

T1 - Novel heterocyclic glucocorticoids

T2 - In vitro profile and in vivo efficacy

AU - Thompson, Christopher F.

AU - Quraishi, Nazia

AU - Ali, Amjad

AU - Tata, James R.

AU - Hammond, Milton L.

AU - Balkovec, James M.

AU - Einstein, Monica

AU - Ge, Lan

AU - Harris, Georgianna

AU - Kelly, Theresa M.

AU - Mazur, Paul

AU - Pandit, Shilpa

AU - Santoro, Joseph

AU - Sitlani, Ayesha

AU - Wang, Chuanlin

AU - Williamson, Joanne

AU - Miller, Douglas K.

AU - Yamin, Ting Ting D.

AU - Thompson, Chris M.

AU - O'Neill, Edward A.

AU - Zaller, Dennis

AU - Forrest, Michael J.

AU - Carballo-Jane, Ester

AU - Luell, Silvi

PY - 2005/4/15

Y1 - 2005/4/15

N2 - A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

AB - A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

KW - Dissociation

KW - Glucocorticoid

KW - Inflammation

KW - Transactivation

KW - Transrepression

UR - https://www.scopus.com/pages/publications/20144387030

U2 - 10.1016/j.bmcl.2005.02.009

DO - 10.1016/j.bmcl.2005.02.009

M3 - Article

C2 - 15808489

AN - SCOPUS:20144387030

SN - 0960-894X

VL - 15

SP - 2163

EP - 2167

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Novel heterocyclic glucocorticoids: In vitro profile and in vivo efficacy

Abstract

Keywords

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